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Issue 37, 2017
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Progress towards the broad use of non-peptide synthetic macrocycles in drug discovery

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Abstract

We discuss progress towards addressing three key questions pertaining to the design of screening libraries of synthetic non-peptidic macrocycles (MCs) for drug discovery: What structural and physicochemical properties of MCs maximize the likelihood of achieving strong and specific binding to protein targets? What features render a protein target suitable for binding MCs, and can this information be used to identify suitable targets for inhibition by MCs? What properties of synthetic MCs confer good pharmaceutical properties, and particularly good aqueous solubility coupled with passive membrane permeability? We additionally discuss how the criteria that define a meaningful MC screening hit are linked to the size of the screening library and the synthetic methodology employed in its preparation.

Graphical abstract: Progress towards the broad use of non-peptide synthetic macrocycles in drug discovery

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Publication details

The article was received on 09 Jan 2017, accepted on 29 Aug 2017 and first published on 29 Aug 2017


Article type: Perspective
DOI: 10.1039/C7OB00056A
Citation: Org. Biomol. Chem., 2017,15, 7729-7735
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    Progress towards the broad use of non-peptide synthetic macrocycles in drug discovery

    A. Whitty, L. A. Viarengo and M. Zhong, Org. Biomol. Chem., 2017, 15, 7729
    DOI: 10.1039/C7OB00056A

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